A functional P2X7 splice variant with an alternative transmembrane domain 1 escapes gene inactivation in P2X7 knock-out mice

J Biol Chem. 2009 Sep 18;284(38):25813-22. doi: 10.1074/jbc.M109.033134. Epub 2009 Jun 22.

Abstract

The ATP-activated P2X7 receptor channel is involved in immune function and inflammatory pain and represents an important drug target. Here we describe a new P2X7 splice variant (P2X7(k)), containing an alternative intracellular N terminus and first transmembrane domain encoded by a novel exon 1 in the rodent P2rx7 gene. Whole cell patch clamp recordings of the rat isoform expressed in HEK293 cells revealed an 8-fold higher sensitivity to the agonist Bz-ATP and much slower deactivation kinetics when compared with the P2X7(a) receptor. Permeability measurements in Xenopus oocytes show a high permeability for N-methyl-D-glucamine immediately upon activation, suggesting that the P2X7(k) channel is constitutively dilated upon opening. The rates of agonist-induced dye uptake and membrane blebbing in HEK cells were also increased. PCR analyses and biochemical analysis by SDS-PAGE and BN-PAGE indicate that the P2X7(k) variant escapes gene deletion in one of the available P2X7(-/-) mice strains and is strongly expressed in the spleen. Taken together, we describe a novel P2X7 isoform with distinct functional properties that contributes to the diversity of P2X7 receptor signaling. Its presence in one of the P2X7(-/-) strains has important implications for our understanding of the role of this receptor in health and disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / analogs & derivatives
  • Adenosine Triphosphate / pharmacology
  • Alternative Splicing / drug effects
  • Alternative Splicing / physiology*
  • Animals
  • Base Sequence
  • Cell Line
  • Cell Membrane Permeability / drug effects
  • Cell Membrane Permeability / physiology
  • Exons / physiology
  • Glutamates / pharmacology
  • Humans
  • Mice
  • Mice, Knockout
  • Molecular Sequence Data
  • Oocytes
  • Platelet Aggregation Inhibitors / pharmacology
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism
  • Protein Structure, Tertiary / physiology
  • Rats
  • Rats, Wistar
  • Receptors, Purinergic P2 / genetics
  • Receptors, Purinergic P2 / metabolism*
  • Receptors, Purinergic P2X7
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*
  • Xenopus laevis

Substances

  • Glutamates
  • P2RX7 protein, human
  • P2rx7 protein, mouse
  • P2rx7 protein, rat
  • Platelet Aggregation Inhibitors
  • Protein Isoforms
  • Receptors, Purinergic P2
  • Receptors, Purinergic P2X7
  • gamma-glutamylmethylamide
  • 3'-O-(4-benzoyl)benzoyladenosine 5'-triphosphate
  • Adenosine Triphosphate

Associated data

  • GENBANK/FJ436444
  • GENBANK/FJ436445